1. Field of the Invention
The present invention relates generally to a composition containing 3-oxygermylpropionic acid (hereinafter 3-OGP for short) having the following general formula:
[(O.sub.1/2).sub.3 GeCH.sub.2 CH.sub.2 COOH]n wherein n=an integer of at least 1 and, more particularly, to a pharmaceutical solid preparation comprising 3-OGP and a low-molecular substance of high solubility in water, which is well solubilized and disintegrated in vivo so that the pharmacological activity of 3-OGP can be much more improved than ever before.
2. Statement of the Prior Art
The pharmacological activity of 3-OGP, because it has complex polymerizability and a variety of applications,.has recently attracted attention, and the antiviral activity of this compound has been known for long as well. In this regard, see JP-P-57-53800, etc.
We have made intensive studies not only of compositions for enabling 3-OGP to maintain its own pharmacological activity stably but of how it acts in vivo as well. We have thus already found that a variety of substances can be effectively used as stabilizers for 3-OGP (see JP-A-61-65819) and that some lactoses can enhance its activity (see JP-A-60-190714).
We have also discovered that some amine salts of 3-OGP are effective (JP-A-1-139587).
Organogermanium compounds have been known for long to have a variety of pharmacological activities not found in other compound systems. However, they are not commercially used as pharmaceutics as yet, because of their disadvantages of differing in action from lot to lot and being unclarified in terms of some specific activities (see JP-P-46-2964 and 58-44677).
In general, when propionic acid drugs are administrated to patients in solid preparation forms, they stimulate the mucosas of the gastrointestinal tracts and are relatively slowly absorbed in the internal organs. In some cases, however, their absorption is delayed or inhibited. For this reason, various forms of drugs such as effervescent ones are now proposed.
However, 3-OGP has some pharmacological problems. For instance, because of its complex polymerizability, 3-OGP is so susceptible to changes in the degree of polymerization due to pressure, moisture, heat, light, etc. that its physico-chemical properties can be likely to vary elusively when manufactured by known drug-making procedures. In addition, the pharmacological activity of 3-OGP is independent on dose and may rather drop at high dose.
So far, we have made studies of how the activity of 3-OGP is stabilized by polymeric compounds, and have now found that when 3-OGP drugs are prepared (in the form of dry tablets) by high-pressure drug-making procedures that are easy to carry out, their activities may often drop, and this is primarily caused by the application of high pressure.
Incidentally, the cytopathogenicity, esp., organopathogenicity and teratogenicity of medicines, toxic substances and radiation appear as side effects in the case of medicines and as social problems such as environmental pollution in the case of toxic substances. However, nothing is done to solve these problems with the exception of some toxicides.
When administrated to those who suffer from organic dysfunctions, esp., patients with hepatitis and nephritis, medicines are likely to produce harmful side effects, causing the patients to suffer from disorders such as anaphylaxy and acute organic dysfunctions and, in the worst case, die.
Drugs having strong cytopathogenicity such as anticancer drugs containing cytotoxins and inhibitors for nucleic acid synthesis have generally strong toxicity to internal organs, and this is the reason why drugs are called a double-edged sword.
A sort of addicts like habitual drinkers and smokers and those who have taken in toxicic substances such as methyl mercury and heavy metal ions suffer from tissular cytopathogenicity and organic disorders, posing social problems. It is considered that all these problems can never be solved without eliminating the causes. Drugs having strong cytopathogenicity or high toxicity to internal organs have similar problems, but they may be eliminated, or at least reduced, by using such drugs in small doses or not using such drugs at all. In some cases, however, these drugs must be urgently administrated to patients with cancer, infectious diseases or other disorders or pregnant women. Thus, there is still a demand for developing how to use such drugs with great safety.
It is an object of this invention to provide a 3-OGP preparation in solid forms which can not only be used with great safety but without degeneration but can also be manufactured simply.
In this connection, it is noted that the 3-OGP used in the present invention is a white acicular crystal having such physicochemical properties as expressed by a specific gravity or density of 2.23, a solubility in water of 1.57 at 20.degree. C. and a melting point of ca. 230.degree. C.